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Dabrafenib

达拉菲尼,GSK-2118436

Dabrafenib (GSK2118436)是一种突变型BRAFV600特异性抑制剂,IC50为0.8 nM,作用于B-Raf(wt)和c-Raf效果低4和6倍。

目录号
EY1600
EY1600
EY1600
EY1600
纯度
98.95%
98.95%
98.95%
98.95%
规格
5 mg
10 mg
50 mg
100 mg
原价
420
720
1700
2600
售价
420
720
1700
2600
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Dabrafenib is a specific inhibitor of BRAF V600 mutants with IC50 values of 0.5nM, 0.6nM and 1.9nM against V600E, V600K and V600D, respectively.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.

    分子式
    C23H20F3N5O2S2
    分子量
    519.56
    CAS号
    1195765-45-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    30 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02700763 Melanoma Other: [18F]dabrafenib molecular imaging University Medical Center Groningen Phase 1 2016-10-01 2016-09-13
    NCT01972347 Melanoma Drug: Dabrafenib|Drug: Trametinib Melanoma Institute Australia Phase 2 2014-10-01 2017-03-21
    NCT01682213 Melanoma Drug: Dabrafenib Memorial Sloan Kettering Cancer Center|National Comprehensive Cancer Network|Novartis Phase 2 2012-09-01 2016-06-07
    NCT02052193 Metastatic Melanoma (Carrying BRAF V600 Mutation) Drug: Dabrafenib|Drug: Vemurafenib University Hospital Tuebingen Phase 2 2014-01-01 2015-07-17
    NCT02231775 Melanoma Drug: Dabrafenib|Drug: Trametinib|Procedure: Surgery M.D. Anderson Cancer Center|Novartis Pharmaceuticals Phase 2 2014-10-01 2017-02-10
    NCT01726738 Stage III Melanoma|Stage IV Melanoma|Unresectable Melanoma|BRAF Mutant Melanoma Drug: BRAF inhibitor dabrafenib and MEK inhibitor trametinib UNC Lineberger Comprehensive Cancer Center|GlaxoSmithKline Phase 2 2012-10-01 2017-03-02
    NCT01721603 BRAFV600E Melanoma Patients Drug: Dabrafenib|Procedure: Gamma Knife Radiosurgery University of California, San Francisco|GlaxoSmithKline Phase 2 2013-04-01 2016-10-28
    NCT02367859 Ameloblastoma|BRAF Gene Mutation Drug: Dabrafenib|Other: Laboratory Biomarker Analysis Stanford University|National Cancer Institute (NCI) Phase 2 2017-04-01 2017-03-01
    NCT02974803 Melanoma|Brain Metastases Drug: Dabrafenib|Drug: Trametinib Canadian Cancer Trials Group|Novartis Phase 2 2016-11-01 2017-03-08
    NCT02447939 Melanoma Drug: Dabrafenib|Drug: Trametinib GlaxoSmithKline Phase 1 2017-05-01 2017-01-25
    NCT01947023 BRAF V600E Mutation Present|BRAF V600K Mutation Present|Metastatic Malignant Neoplasm in the Thyroid Gland|Recurrent Thyroid Gland Carcinoma|Unresectable Thyroid Gland Carcinoma Drug: Dabrafenib|Other: Laboratory Biomarker Analysis|Drug: Lapatinib Ditosylate|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2013-08-01 2016-12-21
    NCT01907802 BRAF Gene Mutation|Hepatic Complication|Renal Failure|Solid Neoplasm Drug: Dabrafenib|Other: Laboratory Biomarker Analysis|Other: Pharmacogenomic Study|Other: Pharmacological Study National Cancer Institute (NCI)|Glaxosmithkline Biologicals S.A. Phase 1 2013-08-01 2017-01-31
    NCT01978236 Melanoma and Brain Metastases Drug: Dabrafenib 150 mg|Drug: Trametinib 2.0 mg GlaxoSmithKline Phase 2 2014-04-01 2016-12-02
    NCT02684058 Anaplastic Astrocytoma|Glioblastoma|Giant Cell Glioblastoma|Gliosarcoma|Anaplastic Oligodendroglioma|Anaplastic Oligoastrocytoma|Anaplastic Ependymoma|Choroid Plexus Carcinoma|Anaplastic Ganglioglioma|Pineal Parenchymal Tumor|Pineoblastoma|Medulloblastoma|PNET|Rhabdoid Tumor|Perineurioma|MPNST|Malignant Meningloma|Anaplastic Hemangiopericytoma Drug: dabrafenib Novartis Pharmaceuticals|Novartis Phase 2 2017-07-17 2017-02-13
    NCT02672358 Non-Small-Cell Lung Cancer Drug: Dabrafenib|Drug: Trametinib Novartis Pharmaceuticals|Novartis Phase 2 2017-10-01 2017-01-03
    NCT02296996 Malignant Melanoma Drug: Dabrafenib + Trametinib Universitair Ziekenhuis Brussel Phase 2 2014-10-01 2016-09-08
    NCT02034110 Cancer Drug: Dabrafenib|Drug: Trametinib GlaxoSmithKline Phase 2 2014-03-01 2017-02-23
    NCT02200562 Stage III or IV Melanoma Drug: ipilimumab and dabrafenib University of Utah Phase 1 2014-12-01 2017-02-27
    NCT01767454 Solid Tumours Drug: Dabrafenib|Drug: Trametinib|Drug: Ipilimumab GlaxoSmithKline Phase 1 2013-02-01 2017-01-23
    NCT01677741 Neoplasms, Brain Drug: Dabrafenib GlaxoSmithKline Phase 1 2013-02-01 2017-03-04
    NCT01584648 Melanoma Drug: dabrafenib|Drug: dabrafenib plus trametinib placebo|Drug: Trametinib GlaxoSmithKline Phase 3 2012-05-01 2017-01-10
    NCT02083354 Cancer Drug: Dabrafenib|Drug: Trametinib GlaxoSmithKline Phase 2 2014-03-01 2017-03-23

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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